4.5 Article

Pyrrolo[3,2-h]quinazolines as Photochemotherapeutic Agents

Journal

CHEMMEDCHEM
Volume 6, Issue 7, Pages 1238-1248

Publisher

WILEY-BLACKWELL
DOI: 10.1002/cmdc.201100085

Keywords

angelicin heteroanalogues; antitumor agents; apoptosis; photochemotherapeutic agents; pyrrolo[3,2-h]quinazolines

Funding

  1. Ministero dell'Istruzione dell'Universite della Ricerca

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Heteroanalogues of angelicin, pyrrolo[3,2-h]quinazolines, were synthesized with the aim of obtaining new potent photochemotherapeutic agents. Many derivatives caused a significant decrease in cell proliferation in several human tumor cell lines after irradiation with UVA light (GI(50) = 15.2-0.2 mu m). Their phototoxicity effected apoptosis in Jurkat cells with the involvement of mitochondria (as determined by the loss of mitochondrial membrane potential and production of reactive oxygen species) and lysosomes. The phototoxicity of these compounds could be explained by lipid peroxidation.

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